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Solvent‐free microwave multicomponent regiospecific synthesis of pyrimido[4,5‐ c ]isoquinolines and evaluation In Vitro of their antifungal properties
Author(s) -
Quiroga Jairo,
Cisneros Carlos,
Insuasty Braulio,
Abonía Rodrigo,
Nogueras Manuel,
Sortino Maximiliano,
Zacchino Susana
Publication year - 2006
Publication title -
journal of heterocyclic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.321
H-Index - 59
eISSN - 1943-5193
pISSN - 0022-152X
DOI - 10.1002/jhet.5570430231
Subject(s) - chemistry , antifungal , in vitro , combinatorial chemistry , microwave , organic chemistry , solvent , microwave irradiation , stereochemistry , biochemistry , microbiology and biotechnology , catalysis , physics , quantum mechanics , biology
The free‐solvent multicomponent reaction under microwave irradiation of 6‐aminopyrimidin‐4(3 H )‐ones ( 1 ) with dimedone ( 2 ) and N,N ‐dimethylformamide dimethylacetal yields the pyrimido[4,5‐ c ]isoquinolinones ( 5a‐j ). In this process, the intermediate of cyclization was isolated. The structure of the synthesized compounds was determined on the basis of nmr measurements, especially by 1 H, 1 H‐, 1 H, 13 C COSY, and DEPT. These compounds showed antifungal in vitro activity particularly against dermatophytes.